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Gene Review

P2ry1  -  purinergic receptor P2Y, G-protein coupled, 1

Rattus norvegicus

Synonyms: ATP receptor, P2Y purinoceptor 1, P2Y1, P2y, P2y1, ...
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Disease relevance of P2ry1


High impact information on P2ry1

  • Radial glial calcium waves occur spontaneously and require connexin hemichannels, P2Y1 ATP receptors, and intracellular IP3-mediated calcium release [6].
  • Of particular interest is the up-regulation of gamma-aminobutyric acid(A) receptor alpha5 subunit, peripheral benzodiazepine receptor, nicotinic acetylcholine receptor alpha7 subunit, P2Y1 purinoceptor, Na(+) channel beta2 subunit, and L-type Ca(2+) channel alpha2delta-1 subunit [7].
  • Time- and concentration-dependent effects of ATP-mediated PGE2 secretion were noted in sinusoidal endothelial cells, whereas the profile of the relative potencies of individual nucleotides was consistent with the presence of P2y and P1 purinergic receptors [8].
  • In osteoclasts purified by micromanipulation, reverse transcription-PCR revealed the presence of P2Y1, P2Y2, and P2Y6 receptor transcripts, and application of agonists for these receptors induced the transient rise of cytosolic calcium [9].
  • Low levels of NF-kappaB activation were observed in untreated rabbit osteoclasts and in those exposed to 2-methylthio ADP (P2Y1 agonist) or ATP or UTP (P2Y2 agonists) [9].

Chemical compound and disease context of P2ry1

  • Whole-cell patch-clamp recordings from cultured rat dorsal root ganglion neurons demonstrated that the P2Y1 receptor agonists adenosine 5'-O-2-thiodiphosphate (ADP-beta-S) and 2-methylthio adenosine 5'-diphosphate (2-MeSADP) inhibit the alpha,beta-methylene adenosine 5'-triphosphate (alpha,beta-meATP)-induced P2X3 receptor-currents [10].
  • Short-term hyperthyroidism modulates the fat-cell adenylate cyclase system at the receptor level (beta-receptor number increased, R-site purinergic-receptor number decreased) and the catalytic subunit of adenylate cyclase [11].
  • Adenosine evoked whole-cell potassium currents and enhanced intracellular free Ca2+ concentration ([Ca2+]i) in superior colliculus neurons through a P2Y purinoceptor linked to a pertussis toxin-insensitive G-protein, possibly Gq-protein, which is involved in a protein kinase C (PKC) activation pathway [12].
  • Moreover, the inhibition of adenylyl cyclase mediated by an endogenous P2Y receptor of C6 glioma cells was not enhanced by expression of the rat P2Y1 receptor [13].
  • 1. Analogues of adenine nucleotides inhibited beta-adrenoceptor-stimulated cyclic AMP accumulation in C6 rat glioma cells with a pharmacological selectivity consistent with that for involvement of a P2Y-purinoceptor [14].

Biological context of P2ry1


Anatomical context of P2ry1


Associations of P2ry1 with chemical compounds

  • Protection by ATP was inhibited by P2 receptor antagonists and was mimicked by P2Y1 receptor agonists but not by adenosine [16].
  • Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors [21].
  • The data provide functional evidence for P2Y1 receptors in the apical membrane of the rat proximal tubule: receptor activation impairs acidification in this nephron segment [21].
  • MRS-2179, a P2Y1 receptor-specific antagonist, abolished the effect of 2MeSADP, whereas theophylline, an antagonist of adenosine (P1) receptors, did not [21].
  • 2-Methylthio-ATP (0.1-10 microM), an agonist that can act at P2Y1 receptors, did not contract arteries or veins, whereas UTP, an agonist at rat P2Y2/P2Y4 receptors, contracted veins (EC(50) = 15 microM) and arteries (EC(50) = 24 microM) [22].

Physical interactions of P2ry1

  • In pure ductal suspensions, ATP activated a metabotropic P2Y1 purinergic receptor coupled to phospholipase C and opened a non-specific cation channel coupled to a P2X7 receptor [23].

Regulatory relationships of P2ry1


Other interactions of P2ry1

  • Of the P2 receptor subtypes examined, P2X1, P2X2 and P2Y1 receptors were found in the smooth muscle layer of intrarenal vessels [20].
  • In addition, staining for P2Y1, -4, and -6 mRNA was shown in the inner nuclear layer, but was absent for the P2Y2 receptor subtype [1].
  • The presence of other ATP receptors such P2Y1 or P2X2/P2X3 heteropolymers in a small fraction of the cells cannot be excluded [25].
  • P2X4, P2Y1 and P2Y2 receptors on rat alveolar macrophages [26].
  • 5. In conclusion, the results show that ionotropic (P2X2) and metabotropic (P2Y1) ATP receptors which occur in the CNS are activated selectively by naturally-occurring adenine dinucleotides which are known to be released with nucleotides from storage vesicles [27].

Analytical, diagnostic and therapeutic context of P2ry1


  1. Expression of P2Y1, P2Y2, P2Y4, and P2Y6 receptor subtypes in the rat retina. Fries, J.E., Wheeler-Schilling, T.H., Guenther, E., Kohler, K. Invest. Ophthalmol. Vis. Sci. (2004) [Pubmed]
  2. P2Y receptor-mediated Ca2+ signalling in cultured rat aortic smooth muscle cells. Pediani, J.D., McGrath, J.C., Wilson, S.M. Br. J. Pharmacol. (1999) [Pubmed]
  3. P2 purinoceptor-mediated dilations in the rat middle cerebral artery after ischemia-reperfusion. Marrelli, S.P., Khorovets, A., Johnson, T.D., Childres, W.F., Bryan, R.M. Am. J. Physiol. (1999) [Pubmed]
  4. The role of P2Y1 purinergic receptors and cytosolic Ca2+ in hypotonically activated osmolyte efflux from a rat hepatoma cell line. Junankar, P.R., Karjalainen, A., Kirk, K. J. Biol. Chem. (2002) [Pubmed]
  5. Effects of extracellular ATP on Fe(2+)-induced cytotoxicity in PC-12 cells. Cheng, Y., Wixom, P., James-Kracke, M.R., Sun, A.Y. J. Neurochem. (1994) [Pubmed]
  6. Calcium waves propagate through radial glial cells and modulate proliferation in the developing neocortex. Weissman, T.A., Riquelme, P.A., Ivic, L., Flint, A.C., Kriegstein, A.R. Neuron (2004) [Pubmed]
  7. Identification of gene expression profile of dorsal root ganglion in the rat peripheral axotomy model of neuropathic pain. Xiao, H.S., Huang, Q.H., Zhang, F.X., Bao, L., Lu, Y.J., Guo, C., Yang, L., Huang, W.J., Fu, G., Xu, S.H., Cheng, X.P., Yan, Q., Zhu, Z.D., Zhang, X., Chen, Z., Han, Z.G., Zhang, X. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  8. Prostanoid secretion by rat hepatic sinusoidal endothelial cells and its regulation by exogenous adenosine triphosphate. Hashimoto, N., Watanabe, T., Shiratori, Y., Ikeda, Y., Kato, H., Han, K., Yamada, H., Toda, G., Kurokawa, K. Hepatology (1995) [Pubmed]
  9. P2Y6 nucleotide receptors activate NF-kappaB and increase survival of osteoclasts. Korcok, J., Raimundo, L.N., Du, X., Sims, S.M., Dixon, S.J. J. Biol. Chem. (2005) [Pubmed]
  10. Metabotropic P2Y1 receptors inhibit P2X3 receptor-channels in rat dorsal root ganglion neurons. Gerevich, Z., Müller, C., Illes, P. Eur. J. Pharmacol. (2005) [Pubmed]
  11. Short-term hyperthyroidism modulates adenosine receptors and catalytic activity of adenylate cyclase in adipocytes. Rapiejko, P.J., Malbon, C.C. Biochem. J. (1987) [Pubmed]
  12. Adenosine evokes potassium currents by protein kinase C activated via a novel signaling pathway in superior colliculus neurons. Nishizaki, T., Ikeuchi, Y. FEBS Lett. (1996) [Pubmed]
  13. Fidelity in functional coupling of the rat P2Y1 receptor to phospholipase C. Schachter, J.B., Boyer, J.L., Li, Q., Nicholas, R.A., Harden, T.K. Br. J. Pharmacol. (1997) [Pubmed]
  14. Potent agonist action of 2-thioether derivatives of adenine nucleotides at adenylyl cyclase-linked P2Y-purinoceptors. Boyer, J.L., O'Tuel, J.W., Fischer, B., Jacobson, K.A., Harden, T.K. Br. J. Pharmacol. (1995) [Pubmed]
  15. Unusual absence of endothelium-dependent or -independent vasodilatation to purines or pyrimidines in the rat renal artery. Knight, G.E., Oliver-Redgate, R., Burnstock, G. Kidney Int. (2003) [Pubmed]
  16. Cytoprotection against oxidative stress-induced damage of astrocytes by extracellular ATP via P2Y1 receptors. Shinozaki, Y., Koizumi, S., Ishida, S., Sawada, J., Ohno, Y., Inoue, K. Glia (2005) [Pubmed]
  17. Expression of P2Y1 receptors in rat taste buds. Kataoka, S., Toyono, T., Seta, Y., Ogura, T., Toyoshima, K. Histochem. Cell Biol. (2004) [Pubmed]
  18. P2X and P2Y purinoceptor expression in pancreas from streptozotocin-diabetic rats. Coutinho-Silva, R., Parsons, M., Robson, T., Lincoln, J., Burnstock, G. Mol. Cell. Endocrinol. (2003) [Pubmed]
  19. Purinergic signalling to rat ovarian smooth muscle: changes in P2X receptor expression during pregnancy. Katugampola, H., Burnstock, G. Cells Tissues Organs (Print) (2004) [Pubmed]
  20. The pattern of distribution of selected ATP-sensitive P2 receptor subtypes in normal rat kidney: an immunohistological study. Turner, C.M., Vonend, O., Chan, C., Burnstock, G., Unwin, R.J. Cells Tissues Organs (Print) (2003) [Pubmed]
  21. Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. Bailey, M.A. Am. J. Physiol. Renal Physiol. (2004) [Pubmed]
  22. Differential localization of P2 receptor subtypes in mesenteric arteries and veins of normotensive and hypertensive rats. Galligan, J.J., Hess, M.C., Miller, S.B., Fink, G.D. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  23. Purines, a new class of agonists in salivary glands? Dehaye, J.P., Moran, A., Marino, A. Arch. Oral Biol. (1999) [Pubmed]
  24. Purinergic P2y receptors stimulate renin secretion by rat renal cortical slices. Churchill, P.C., Ellis, V.R. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  25. Functional ATP receptors in rat anterior pituitary cells. Villalobos, C., Alonso-Torre, S.R., Núñez, L., García-Sancho, J. Am. J. Physiol. (1997) [Pubmed]
  26. P2X4, P2Y1 and P2Y2 receptors on rat alveolar macrophages. Bowler, J.W., Bailey, R.J., North, R.A., Surprenant, A. Br. J. Pharmacol. (2003) [Pubmed]
  27. Selectivity and activity of adenine dinucleotides at recombinant P2X2 and P2Y1 purinoceptors. Pintor, J., King, B.F., Miras-Portugal, M.T., Burnstock, G. Br. J. Pharmacol. (1996) [Pubmed]
  28. P2X2 and P2Y1 immunofluorescence in rat neostriatal medium-spiny projection neurones and cholinergic interneurones is not linked to respective purinergic receptor function. Scheibler, P., Pesic, M., Franke, H., Reinhardt, R., Wirkner, K., Illes, P., Nörenberg, W. Br. J. Pharmacol. (2004) [Pubmed]
  29. Expression profiles of P2-receptor isoforms P2Y1 and P2Y2 in the rat lens. Merriman-Smith, R., Tunstall, M., Kistler, J., Donaldson, P., Housley, G., Eckert, R. Invest. Ophthalmol. Vis. Sci. (1998) [Pubmed]
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